Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII.

Rami M; Maresca A; Smaine FZ; Montero JL; Scozzafava A; Winum JY; Supuran CT

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Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII.

机译：结合有硼唑烷酮部分的磺酰胺是跨膜，与肿瘤相关的碳酸酐酶同工型IX和XII的有效抑制剂。

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A new series of sulfonamides was synthesized by the reaction of the boroxazolidone complex of l-lysine with isothiocyanates incorporating sulfamoyl moieties and diverse organic scaffolds. The obtained thioureas have been investigated as inhibitors of four physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IX and XII. Inhibition between the low nanomolar to the micromolar range has been observed against them, with several low nanomolar and tumor-CA selective inhibitors detected. These boron-containing compounds might be useful for the management of hypoxic tumors overexpressing hCA IX/XII by means of boron neutron capture therapy, a technique not investigated so far with inhibitors of this enzyme.

机译：通过使l-赖氨酸的硼恶唑烷酮配合物与结合了氨磺酰基部分和各种有机支架的异硫氰酸酯反应，合成了一系列新的磺酰胺。已经研究了获得的硫脲作为四种生理相关的人碳酸酐酶（hCA，EC 4.2.1.1）同工型hCA I，II，IX和XII的抑制剂。已经观察到低纳摩尔至微摩尔范围之间对它们的抑制作用，并检测到几种低纳摩尔和肿瘤CA选择性抑制剂。这些含硼化合物可能通过硼中子俘获疗法用于治疗过表达hCA IX / XII的低氧肿瘤，该技术迄今为止尚未对该酶抑制剂进行过研究。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共5页
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Rami M; Maresca A; Smaine FZ; Montero JL; Scozzafava A; Winum JY; Supuran CT;
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1. Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. [J] . Rami M, Maresca A, Smaine FZ, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：结合有硼唑烷酮部分的磺酰胺是跨膜，与肿瘤相关的碳酸酐酶同工型IX和XII的有效抑制剂。
2. Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. [J] . Carta F, Garaj V, Maresca A, Bioorganic and medicinal chemistry . 2011,第10期

机译：与胞质同工型I和II相比，掺入1,3,5-三嗪部分的磺酰胺有选择地并有效地抑制了碳酸酐酶跨膜同工型IX，XII和XIV：溶液和X射线晶体学研究。
3. Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. [J] . Carta F, Garaj V, Maresca A, Bioorganic and medicinal chemistry . 2011,第10期

机译：与胞质同工型I和II相比，掺入1,3,5-三嗪部分的磺酰胺有选择地并有效地抑制了碳酸酐酶跨膜同工型IX，XII和XIV：溶液和X射线晶体学研究。
4. QSAR AND DOCKING STUDIES ON TRIAZOLE BENZENE SULFONAMIDES WITH HUMAN CARBONIC ANHYDRASE IX INHIBITORY ACTIVITY [C] . Gopinath P., Kathiravan M.K. Conference on Drug Design and Discovery Technologies . 2020

机译：用人碳酸酐酶IX抑制活性对三唑苯磺胺酰胺的QSAR和对接研究
5. Development of a DNA Aptamer that Specifically Inhibits Human Carbonic Anhydrase II [D] . Karim, Afroz 2018

机译：特异性抑制人类碳酸酐酶II的DNA适体的开发
6. Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII [O] . Kübra Demir-Yazıcı, Silvia Bua, Nurgül Mutlu Akgüneş, 2019

机译：包含磺酰胺部分的吲哚基Hy作为肿瘤相关人类碳酸酐酶异构体IX和XII的选择性抑制剂。
7. Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII [O] . Kübra Demir-Yazıcı, Silvia Bua, Nurgül Mutlu Akgüneş, 2019

机译：基于吲哚的腙，其含磺酰胺部分作为肿瘤相关人类碳酸酐酶同种型IX和XII的选择性抑制剂

Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII.

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